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TUL01101
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TUL01101图片
CAS NO:2411222-97-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
TUL01101 是一种有效,选择性和具有口服活性的JAK1抑制剂,对 JAK1,JAK2,JAK3 和 TYK2 的IC50值分别为 3,37,1517 和 36 nM。TUL01101 可用于类风湿性关节炎的研究。
生物活性

TUL01101 is a potent, selective and orally activeJAK1inhibitor, with anIC50s of 3, 37, 1517 and 36 nM forJAK1,JAK2,JAK3, andTYK2, respectively. TUL01101 can be used for the research of rheumatoid arthritis[1].

IC50& Target[1]

JAK1

3 nM (IC50)

JAK2

37 nM (IC50)

JAK3

1517 nM (IC50)

Tyk2

36 nM (IC50)

体外研究
(In Vitro)

TUL01101 (pretreatment for 1 h) inhibits cytokine-induced pSTAT in human whole blood assay[1].

体内研究
(In Vivo)

TUL01101 (1-30 mg/kg; p.o. twice daily for 14 d) inhibits rheumatoid arthritis in the rat adjuvant-induced arthritis (AIA) model[1].
TUL01101 (15 mg/kg; p.o. twice daily for 14 d) inhibits rheumatoid arthritis in collagen-induced arthritis models[1].
TUL01101 (15 mg/kg; p.o.) exhibits T1/2of 2.01 h, Cmaxof 5105 nM, and oral bioavailability of 38.1% in mice[1].
TUL01101 (10 mg/kg; p.o.) exhibits T1/2of 3.06 h, Cmaxof 4965 nM, and oral bioavailability of 121% in rats[1].
TUL01101 (5 mg/kg; p.o.) exhibits T1/2of 4.49 h, Cmaxof 2750 nM, and oral bioavailability of 106.5% in dogs[1].

Animal Model:Rat adjuvant-induced arthritis (AIA) model[1]
Dosage:1, 3, 10, 30 mg/kg
Administration:Orally administered twice daily for 14 days
Result:Decreased the incidence in a dose-dependent manner.
分子量

429.46

Formula

C22H25F2N5O2

CAS 号

2411222-97-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.